alpha-Fluoromethyl histidine. Inhibition of histidine decarboxylase in pylorus ligated rat

Biochem Pharmacol. 1983 May 15;32(10):1553-6. doi: 10.1016/0006-2952(83)90326-x.

Abstract

alpha-Fluoromethyl histidine is an irreversible inhibitor of histidine decarboxylase. The injection of a single dose to pyloric-ligated rats inhibits gastric mucosal histidine decarboxylase in a dose-dependent manner but does not modify histamine content and gastric acid secretion even at the highest dose used. Administration of cimetidine increases histidine decarboxylase activity, decreases histamine level in gastric mucosa and inhibits gastric acid secretion. The co-administration of alpha-fluoromethyl histidine blocks the augmentation in enzyme activity, maintains lowered histamine level and prolongs the antisecretory action of cimetidine.

MeSH terms

  • Animals
  • Carboxy-Lyases / antagonists & inhibitors*
  • Cimetidine / pharmacology
  • Dose-Response Relationship, Drug
  • Gastric Acid / metabolism
  • Gastric Mucosa / enzymology
  • Histamine / metabolism
  • Histidine / analogs & derivatives*
  • Histidine Decarboxylase / antagonists & inhibitors*
  • Ligation
  • Male
  • Methylhistidines / pharmacology*
  • Pylorus / physiology
  • Pylorus / surgery
  • Rats
  • Rats, Inbred Strains

Substances

  • Methylhistidines
  • Histidine
  • alpha-fluoromethylhistidine
  • Cimetidine
  • Histamine
  • Carboxy-Lyases
  • Histidine Decarboxylase